Energy generation is a promising area of drug discovery for both bacterial pathogens and parasites. Type II NADH dehydrogenase (NDH-2), a vital respiratory membrane protein, has attracted attention as a target for the development of new antitubercular and antimalarial agents. To date, however, no potent, specific inhibitors have been identified. Here, we performed a site-directed screening technique, tethering-fragment based drug discovery, against wild-type and mutant forms of NDH-2 containing engineered active-site cysteines. Inhibitory fragments displayed IC50 values between 3 and 110 μM against NDH-2 mutants. Possible binding poses were investigated by in silico modelling, providing a basis for optimisation of fragment binding and improved potency against NDH-2.
Pharmacology, Toxicology and Pharmaceutical Science
3
10%
Agricultural and Biological Sciences
2
7%
Medicine and Dentistry
1
3%
Other
0
0%
Unknown
10
33%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 7. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 29 May 2021.
All research outputs
#7,063,613
of 33,779,198 outputs
Outputs from Bioorganic & Medicinal Chemistry Letters
#5,009
of 17,123 outputs
Outputs of similar age
#98,750
of 373,308 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry Letters
#25
of 109 outputs
Altmetric has tracked 33,779,198 research outputs across all sources so far. Compared to these this one has done well and is in the 78th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 17,123 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.1. This one has gotten more attention than average, scoring higher than 70% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 373,308 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 73% of its contemporaries.
We're also able to compare this research output to 109 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 77% of its contemporaries.
